6-[2-(4-aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones:: Dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors

被引：26

作者：

Bromidge, Steven M. ^{[1
]}

Bertani, Barbara ^{[2
]}

Borriello, Manuela ^{[2
]}

Faedo, Stefania ^{[2
]}

Gordon, Laurie J. ^{[1
]}

Granci, Enrica ^{[2
]}

Hill, Matthew ^{[1
]}

Marshall, Howard R. ^{[1
]}

Stasi, Luigi P. ^{[2
]}

Zucchelli, Valeria ^{[2
]}

Merlo, Giancarlo ^{[2
]}

Vesentini, Alessia ^{[2
]}

Watson, Jeannette M. ^{[1
]}

Zonzini, Laura ^{[2
]}

机构：

[1] GlaxoSmithKline Inc, Neurosci CEDD, Harlow CM19 5AW, Essex, England

[2] GlaxoSmithKline Inc, Neurosci CEDD, Med Res Ctr, I-37135 Verona, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 20期

关键词：

5-HT1A/1B/1D receptor antagonists; serotonin reuptake inhibitors; 5-HT1; autoreceptors; antidepressant;

D O I：

10.1016/j.bmcl.2008.08.084

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Investigation of a series 6-[2-(4-aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones has led to the discovery of potent 5-HT1A/1B/1D receptor antagonists with and without additional SerT affinity. Modulation of the different target activities gave compounds with a range of profiles suitable for further in vivo characterization. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：5653 / 5656

页数：4

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